PDE6 inhibitor
Phosphodiesterase-6 inhibitor
- Off-target inhibition of retinal PDE6 in the phototransduction cascade
- The basis of blue-tinged vision
- Weak PDE5-over-PDE6 selectivity is the stated basis for this and for light sensitivity
- Sildenafil ~10-fold and vardenafil >15-fold selective; tadalafil 700-fold and avanafil >100-fold, which is why they lack the visual signature
Drugs with this mechanism (2)
- Sildenafil — The first PDE5 inhibitor (Viagra); also treats pulmonary hypertension.
- Vardenafil — PDE5 inhibitor for erectile dysfunction.
Self-check
- Where does off-target PDE6 inhibition act?
The retina’s phototransduction cascade. - Which listed PDE5 inhibitor has about 700-fold PDE5-over-PDE6 selectivity?
Tadalafil.
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